2. T6167923

T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.

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T6167923 Chemical Structure

T6167923 Chemical Structure

CAS No. : 2437475-16-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 565 In-stock
Solution
10 mM * 1 mL in DMSO USD 565 In-stock
Solid
5 mg USD 560 In-stock
10 mg USD 840 In-stock
25 mg USD 1500 In-stock
50 mg USD 2100 In-stock
100 mg USD 2940 In-stock
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Based on 11 publication(s) in Google Scholar

T6167923 Related Antibodies

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Description

T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively[1][2].

IC50 & Target

IC50: 2.7 μM (IFN-γ), 2.9 μM (IL-1β), 2.66 μM (IL-6), 2.66 μM (TNF-α)[2]
In Vitro

T6167923 (0-500 μM; 20 h) inhibits the pro-inflammatory cytokine response of staphylococcal enterotoxin B (SEB) in peripheral blood mono nuclear cells[2].
T6167923 (10-500 μM; 2 h) inhibits secreted alkaline phosphatase response (SEAP) expression in HEK 293T cells[2].
T6167923 (100 μM; 16 h) binds to TIR protein and reduced the inhibitory effect on MyD88-signaling[2].
T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

T6167923 Related Antibodies

Cell Viability Assay[2]

Cell Line: Peripheral blood mono nuclear cells
Concentration: 0-500 μM
Incubation Time: 20 hours
Result: Dose-dependently attenuated the response of SEB to TNF-α, INF-γ, IL-6, and IL-1β with IC50s of 2.66, 2.7, 2.66 and 2.9 μM in peripheral blood mono nuclear cells.

Cell Viability Assay[2]

Cell Line: HEK 293T cell line
Concentration: 10-500 μM
Incubation Time: 2 hours
Result: Dose-dependently inhibited lipo-polysaccharide (LPS) induced MyD88-mediated NF-kB driven SEAP expression in HEK 293T cells with IC50s in the range of 40–50 μM.

Cell Viability Assay[2]

Cell Line: HEK 293T cell line
Concentration: 100 μM
Incubation Time: 16 hours
Result: Specifically targeted MyD88 and dose-denpendently with TIR protein to reduced the inhibitory effect of MyD88-signaling.

Western Blot Analysis[2]

Cell Line: HEK 293-I3A cells with MyD88 knockout
Concentration: 1-500 μM
Incubation Time: 13 hours
Result: Dose-dependently inhibited TIR domain-mediated dimerization of full-length MyD88 and the recombinant TIR domain protein.
In Vivo

T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 16-20 week-old BALB/c mice with LPS potentiation model[2]
Dosage: 0.17 and 1 mg
Administration: Intraperitoneal injection; 0.17 and 1 mg once
Result: Dose-dependently showed a therapeutic efficacy against SEB intoxication.
Molecular Weight

458.39

Formula

C17H20BrN3O3S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

BrC1=CC(S(=O)(N2CCN(C(N[C@H](C3=CC=CS3)C)=O)CC2)=O)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (545.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1815 mL 10.9077 mL 21.8155 mL
5 mM 0.4363 mL 2.1815 mL 4.3631 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1815 mL 10.9077 mL 21.8155 mL 54.5387 mL
5 mM 0.4363 mL 2.1815 mL 4.3631 mL 10.9077 mL
10 mM 0.2182 mL 1.0908 mL 2.1815 mL 5.4539 mL
15 mM 0.1454 mL 0.7272 mL 1.4544 mL 3.6359 mL
20 mM 0.1091 mL 0.5454 mL 1.0908 mL 2.7269 mL
25 mM 0.0873 mL 0.4363 mL 0.8726 mL 2.1815 mL
30 mM 0.0727 mL 0.3636 mL 0.7272 mL 1.8180 mL
40 mM 0.0545 mL 0.2727 mL 0.5454 mL 1.3635 mL
50 mM 0.0436 mL 0.2182 mL 0.4363 mL 1.0908 mL
60 mM 0.0364 mL 0.1818 mL 0.3636 mL 0.9090 mL
80 mM 0.0273 mL 0.1363 mL 0.2727 mL 0.6817 mL
100 mM 0.0218 mL 0.1091 mL 0.2182 mL 0.5454 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

T61679232437475-16-4T 6167923T-6167923Inhibitorinhibitorinhibit

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